Dronabinol Compositions with Room-Temperature Oxidation Stability
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Solution Overview
Problem
Delta-9-tetrahydrocannabinol (THC) compositions deteriorate upon storage, leading to decreased effectiveness and purity due to oxidation and degradation, necessitating refrigerated storage and limited shelf life, and existing stabilizers like palmitoyl ascorbic acid cause instability and unpleasant odor.
Innovation Solution
A composition comprising THC in a lipophilic carrier with additives such as rosemary extract, eugenol, vitamin E, or lecithin, which are dissolved without heating, maintaining stability at room temperature and preventing oxidation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If THC is stored at room temperature, then ease of operation is improved, but stability deteriorates due to oxidation and degradation
Solution Approach 1:
The patent introduces phenolic antioxidants (such as BHA, BHT, or rosemary extract) as intermediary substances that mediate between THC and oxygen. These antioxidants preferentially react with oxygen or free radicals, protecting THC from oxidation and degradation, thereby enabling stable room temperature storage without refrigeration.
Solution Approach 2:
The patent changes the chemical composition parameters of the THC preparation by adding specific antioxidants at controlled concentrations (0.01-0.5% w/v). This parameter modification fundamentally alters the oxidation resistance of the formulation, allowing it to maintain stability at room temperature rather than requiring refrigeration.
2Stability of the object's composition
If palmitoyl ascorbic acid is used as a stabilizer, then THC stability is improved, but solubility deteriorates requiring heating to 85°C
Solution Approach 1:
The patent extracts or replaces the problematic stabilizer (palmitoyl ascorbic acid) with superior alternatives (phenolic antioxidants like BHA, BHT, or rosemary extract). These replacement antioxidants provide equivalent or better stabilization without the solubility issues, eliminating the need for high-temperature processing.
Solution Approach 2:
The patent changes the chemical nature of the stabilizer from a water-soluble vitamin derivative (palmitoyl ascorbic acid) to lipid-soluble phenolic compounds. This parameter change in chemical compatibility with the oily carrier enables complete dissolution at room temperature while maintaining or enhancing stabilization efficacy.
3Stability of the object's composition
If palmitoyl ascorbic acid is used as a stabilizer, then THC stability is improved, but harmful factors increase due to unpleasant odor and taste
Solution Approach 1:
The patent removes the source of unpleasant odor and taste (palmitoyl ascorbic acid) and replaces it with phenolic antioxidants that are odorless or have pleasant aromatic properties. This substitution eliminates the harmful sensory effects while preserving the stabilization function.
Solution Approach 2:
The patent converts the potential harm of oxidation (which causes degradation) into a benefit by using antioxidants that not only prevent oxidation but also contribute positive sensory properties. For example, rosemary extract provides both stabilization and a pleasant herbal aroma, turning a potential negative into a positive attribute.
4Stability of the object's composition
If THC compositions are refrigerated, then stability is improved, but loss of time increases due to limited shelf life after opening
Solution Approach 1:
The patent applies preliminary protection by incorporating antioxidants into the formulation before storage. This pre-established protective system actively prevents oxidation from the moment of opening, extending the usable shelf life without requiring refrigeration and eliminating the time loss associated with temperature management.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The composition maintains at least 80% THC in undegraded form for up to 12 months at room temperature, ensuring therapeutic efficacy and avoiding odor issues.
Implementation Method 1
THC is known to deteriorate upon storage so that the effective concentration decreases upon storage and moreover, its purity is compromised due to the appearance of degradation products
Data Source
AI summary
The present invention relates to a composition comprising delta-9-tetrahydrocannabinol (THC, dronabinol), a lipophilic carrier such as medium chain triglycerides (MCT) and at least one additive. The present invention also relates to pharmaceutical compositions comprising said compositions. In particular, the present invention relates to a room temperature stable composition of THC in a lipophilic carrier. Furthermore, the present invention relates to a method for stabilizing THC in a composition and the use of specific additives for the stabilization of THC.